WO2009155017A2 - Nouveaux azabenzoxazoles substitués - Google Patents

Nouveaux azabenzoxazoles substitués Download PDF

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Publication number
WO2009155017A2
WO2009155017A2 PCT/US2009/045376 US2009045376W WO2009155017A2 WO 2009155017 A2 WO2009155017 A2 WO 2009155017A2 US 2009045376 W US2009045376 W US 2009045376W WO 2009155017 A2 WO2009155017 A2 WO 2009155017A2
Authority
WO
WIPO (PCT)
Prior art keywords
oxazolo
pyridin
fluoro
pyridine
compound according
Prior art date
Application number
PCT/US2009/045376
Other languages
English (en)
Other versions
WO2009155017A3 (fr
Inventor
James C. Barrow
Scott Harrison
James Mulhearn
Cyrille Sur
David L. Williams
Scott Wolkenberg
Original Assignee
Merck & Co., Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Priority to US12/995,314 priority Critical patent/US8530483B2/en
Priority to JP2011511794A priority patent/JP2011524864A/ja
Priority to CA2725940A priority patent/CA2725940A1/fr
Priority to AU2009260519A priority patent/AU2009260519A1/en
Priority to ES09767329.7T priority patent/ES2554772T3/es
Priority to EP09767329.7A priority patent/EP2300481B1/fr
Publication of WO2009155017A2 publication Critical patent/WO2009155017A2/fr
Publication of WO2009155017A3 publication Critical patent/WO2009155017A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Nouveaux composés se liant aux amyloïdes et méthodes de mesure de leurs effets consistant à mesurer des changements de niveau des plaques amyloïdes chez des patients vivants. Plus précisément, méthode d'utilisation desdits composés comme traceurs dans le cadre d'une tomographie par émission de positions visant à étudier des dépôts d'amyloïdes dans le cerveau in vivo pour le diagnostic de la maladie d'Alzheimer. Ainsi, cette invention concerne l'utilisation des nouveaux composés qui se lient aux amyloïdes comme outil de diagnostic. De plus, l'invention concerne une méthode de mesure de l'efficacité clinique d'agents thérapeutiques de la maladie d'Alzheimer. Spécifiquement, l'invention porte sur des nouveau dérivés d'azabenzoxazole substitués aryle ou hétéroaryle, des compositions et des utilisations thérapeutiques ainsi que des méthodes de fabrication de tels composés.
PCT/US2009/045376 2008-05-30 2009-05-28 Nouveaux azabenzoxazoles substitués WO2009155017A2 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
US12/995,314 US8530483B2 (en) 2008-05-30 2009-05-28 Substituted azabenzoxazoles
JP2011511794A JP2011524864A (ja) 2008-05-30 2009-05-28 新規な置換されたアザベンゾオキサゾール
CA2725940A CA2725940A1 (fr) 2008-05-30 2009-05-28 Nouveaux azabenzoxazoles substitues
AU2009260519A AU2009260519A1 (en) 2008-05-30 2009-05-28 Novel substituted azabenzoxazoles
ES09767329.7T ES2554772T3 (es) 2008-05-30 2009-05-28 Azabenzoxazoles sustituidos novedosos
EP09767329.7A EP2300481B1 (fr) 2008-05-30 2009-05-28 Nouveaux azabenzoxazoles substitués

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US13039908P 2008-05-30 2008-05-30
US61/130,399 2008-05-30
US19802208P 2008-10-31 2008-10-31
US61/198,022 2008-10-31

Publications (2)

Publication Number Publication Date
WO2009155017A2 true WO2009155017A2 (fr) 2009-12-23
WO2009155017A3 WO2009155017A3 (fr) 2010-02-18

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/045376 WO2009155017A2 (fr) 2008-05-30 2009-05-28 Nouveaux azabenzoxazoles substitués

Country Status (7)

Country Link
US (1) US8530483B2 (fr)
EP (1) EP2300481B1 (fr)
JP (1) JP2011524864A (fr)
AU (1) AU2009260519A1 (fr)
CA (1) CA2725940A1 (fr)
ES (1) ES2554772T3 (fr)
WO (1) WO2009155017A2 (fr)

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WO2011090738A3 (fr) * 2009-12-29 2011-11-24 Dana-Farber Cancer Institute, Inc. Inhibiteurs de kinase raf de type ii
DE102010045797A1 (de) 2010-09-20 2012-03-22 Klinikum Darmstadt Gmbh Verbindungen für die Diagnostik neurodegenerativer Erkrankungen am Riechepithel
WO2012041292A2 (fr) 2010-09-20 2012-04-05 Klinikum Darmstadt Gmbh Composés pour le diagnostic de maladies neurodégénératives sur la rétine
US8242133B2 (en) * 2008-04-21 2012-08-14 Sumitomo Chemical Company, Limited Arthropod pest control compositions comprising substituted oxazolo [5,4-b ] pyridines
WO2013004826A1 (fr) * 2011-07-07 2013-01-10 Sanofi Dérivés d'acide carboxylique contenant un cycle oxazolo-[5,4-b]-pyridine
WO2013004824A1 (fr) * 2011-07-07 2013-01-10 Sanofi Dérivés d'acide carboxylique contenant un cycle oxazolo-[4,5-c]-pyridine
KR20140061386A (ko) * 2011-07-07 2014-05-21 사노피 옥사졸로［４，５­ｃ］피리딘 환을 갖는 카복실산 유도체
KR20140061385A (ko) * 2011-07-07 2014-05-21 사노피 옥사졸로［５，４­ｄ］피리미딘 환을 갖는 카복실산 유도체
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US9505784B2 (en) 2009-06-12 2016-11-29 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
KR20160137108A (ko) * 2015-05-22 2016-11-30 한국과학기술연구원 벤조옥사졸 또는 벤조티아졸 화합물, 그의 제조, 및 용도
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2017153601A1 (fr) 2016-03-11 2017-09-14 Ac Immune Sa Composés bicycliques pour diagnostic et traitement
CN107207530A (zh) * 2014-12-02 2017-09-26 拜耳作物科学股份公司 作为害虫防治剂的双环化合物
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2019234243A1 (fr) 2018-06-08 2019-12-12 Ac Immune Sa Nouveaux composés pour diagnostic
WO2020012422A1 (fr) 2018-07-13 2020-01-16 Richter Gedeon Nyrt. Dérivés de spirochromane
WO2020012424A1 (fr) 2018-07-13 2020-01-16 Richter Gedeon Nyrt. Dérivés d'(aza)indole substitués
US10550121B2 (en) 2015-03-27 2020-02-04 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10906889B2 (en) 2013-10-18 2021-02-02 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
US11040957B2 (en) 2013-10-18 2021-06-22 Dana-Farber Cancer Institute, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
US11142507B2 (en) 2015-09-09 2021-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2021224489A1 (fr) 2020-05-07 2021-11-11 Ac Immune Sa Nouveaux composés pour diagnostic
WO2023084000A1 (fr) 2021-11-10 2023-05-19 Ac Immune Sa Dérivés de 4h-imidazo[1,5-b]pyrazole à des fins de diagnostic
WO2023083961A1 (fr) 2021-11-10 2023-05-19 Ac Immune Sa Dérivés du dihydropyrrolo[3,4-c]pyrazole et leur utilisation à des fins de diagnostic
WO2023083998A1 (fr) 2021-11-10 2023-05-19 Ac Immune Sa Dérivés du dihydropyrrolo[3,4c]-pyrazole et leur utilisation à des fins de diagnostic
WO2023112056A1 (fr) 2021-12-17 2023-06-22 Pi Industries Ltd. Nouveaux composés de pyridine carboxamide bicycliques fusionnés substitués pour lutter contre des champignons phytopathogènes

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ES2818107T3 (es) * 2014-08-29 2021-04-09 Chdi Foundation Inc Sondas para obtener imágenes de la proteína huntingtina
HRP20211778T1 (hr) * 2014-08-29 2022-03-18 Chdi Foundation, Inc. Kontrastna sredstva za slikovnu dijagnostiku huntingtin proteina
JP6831802B2 (ja) * 2018-01-12 2021-02-17 上海富吉医療器械有限公司Ｓｈａｎｇｈａｉ Ｃｈａｒｔｗｅｌｌ Ｍｅｄｉｃａｌ Ｉｎｓｔｒｕｍｅｎｔ Ｃｏ．， Ｌｔｄ． 放射性核種標識化合物及びこれを含有するイメージング剤

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Cited By (59)

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Publication number Priority date Publication date Assignee Title
US8324387B2 (en) 2008-04-21 2012-12-04 Sumitomo Chemical Company, Limited Substituted Oxazolo[5,4-b]pyridines
US8609705B2 (en) 2008-04-21 2013-12-17 Sumitomo Chemical Company, Limited Fused heterocyclic compounds, and compositions thereof, for use in arthropod pest control
US8445522B2 (en) 2008-04-21 2013-05-21 Sumitomo Chemical Company, Limited Substituted 2-(4-pyridyl)benzoxazoles, and compositions thereof, for use in arthropod pest control
US8242133B2 (en) * 2008-04-21 2012-08-14 Sumitomo Chemical Company, Limited Arthropod pest control compositions comprising substituted oxazolo [5,4-b ] pyridines
US9505784B2 (en) 2009-06-12 2016-11-29 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
WO2011090738A3 (fr) * 2009-12-29 2011-11-24 Dana-Farber Cancer Institute, Inc. Inhibiteurs de kinase raf de type ii
US11826365B2 (en) 2009-12-29 2023-11-28 Dana-Farber Cancer Institute, Inc. Type II raf kinase inhibitors
AU2016201096B2 (en) * 2009-12-29 2017-08-31 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
US9358231B2 (en) 2009-12-29 2016-06-07 Dana-Farber Cancer Institute, Inc. Type II RAF kinase inhibitors
AU2010343102B2 (en) * 2009-12-29 2016-03-24 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
WO2012041292A2 (fr) 2010-09-20 2012-04-05 Klinikum Darmstadt Gmbh Composés pour le diagnostic de maladies neurodégénératives sur la rétine
WO2012037928A2 (fr) 2010-09-20 2012-03-29 Klinikum Darmstadt Gmbh Composés pour le diagnostic de maladies neurodégénératives sur l'épithélium olfactif
DE102010045797A1 (de) 2010-09-20 2012-03-22 Klinikum Darmstadt Gmbh Verbindungen für die Diagnostik neurodegenerativer Erkrankungen am Riechepithel
RU2609008C2 (ru) * 2011-07-07 2017-01-30 Санофи ПРОИЗВОДНЫЕ КАРБОНОВЫХ КИСЛОТ С ОКСАЗОЛО[5, 4-d]ПИРИМИДИНОВЫМ ЦИКЛОМ
RU2609003C2 (ru) * 2011-07-07 2017-01-30 Санофи Производные карбоновых кислот, имеющие оксазоло[4,5-d]пиримидиновое кольцо
US8907093B2 (en) 2011-07-07 2014-12-09 Sanofi Carboxylic acid derivatives having an oxazolo[4,5-c]pyridine ring
KR20140061386A (ko) * 2011-07-07 2014-05-21 사노피 옥사졸로［４，５­ｃ］피리딘 환을 갖는 카복실산 유도체
KR20140061384A (ko) * 2011-07-07 2014-05-21 사노피 옥사졸로［５，４­ｂ］피리딘 환을 갖는 카복실산 유도체
CN103781791B (zh) * 2011-07-07 2016-04-06 赛诺菲 具有噁唑并[4,5-c]吡啶环的羧酸衍生物
CN103781791A (zh) * 2011-07-07 2014-05-07 赛诺菲 具有噁唑并[4,5-c]吡啶环的羧酸衍生物
WO2013004826A1 (fr) * 2011-07-07 2013-01-10 Sanofi Dérivés d'acide carboxylique contenant un cycle oxazolo-[5,4-b]-pyridine
CN103781790A (zh) * 2011-07-07 2014-05-07 赛诺菲 具有噁唑并[5,4-b]吡啶环的羧酸衍生物
KR20140061385A (ko) * 2011-07-07 2014-05-21 사노피 옥사졸로［５，４­ｄ］피리미딘 환을 갖는 카복실산 유도체
WO2013004824A1 (fr) * 2011-07-07 2013-01-10 Sanofi Dérivés d'acide carboxylique contenant un cycle oxazolo-[4,5-c]-pyridine
RU2609002C2 (ru) * 2011-07-07 2017-01-30 Санофи ПРОИЗВОДНЫЕ КАРБОНОВЫХ КИСЛОТ С ОКСАЗОЛО[5,4-b] ПИРИДИНОВЫМ КОЛЬЦОМ
RU2609004C2 (ru) * 2011-07-07 2017-01-30 Санофи Производные карбоновых кислот с оксазоло[4,5-с]пиридиновым циклом
US8580816B2 (en) 2011-07-07 2013-11-12 Sanofi Carboxylic acid derivatives having an oxazolo[5,4-b]pyridine ring
US10144730B2 (en) 2011-11-17 2018-12-04 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US10981903B2 (en) 2011-11-17 2021-04-20 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10787436B2 (en) 2012-10-18 2020-09-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US11040957B2 (en) 2013-10-18 2021-06-22 Dana-Farber Cancer Institute, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
US10906889B2 (en) 2013-10-18 2021-02-02 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
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AU2009260519A1 (en) 2009-12-23
CA2725940A1 (fr) 2009-12-23
US8530483B2 (en) 2013-09-10
US20110085985A1 (en) 2011-04-14
JP2011524864A (ja) 2011-09-08
ES2554772T3 (es) 2015-12-23
EP2300481A2 (fr) 2011-03-30
EP2300481B1 (fr) 2015-09-30

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